A kind of docetaxel polymer nano injection and preparation method thereof

Abstract

The invention provides a docetaxel polymer nano-injection, comprising the following components: modified docetaxel, a photosensitizer and a pH-sensitive block; the modified docetaxel is cross-linked by a shell polymer Coating modification; the modified docetaxel and the photosensitizer are connected through an acid-sensitive bond; the pH-sensitive block is coated outside the photosensitizer. The invention also provides a preparation method of the docetaxel polymer nano injection. The present invention enables docetaxel to have higher water solubility and higher stability, is not easy to cause systemic toxic and side effects due to sudden release, and can be released slowly. At the same time, the combined treatment of chemotherapy and phototherapy can effectively improve the effect on tumor cells. treatment effect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a docetaxel polymer nano-injection and a preparation method thereof. Background technique [0002] Taxanes play an important role in the treatment of various solid tumors; docetaxel, a second-generation semi-synthetic taxane derivative, is approximately twice as potent as paclitaxel in participating in microtubule depolymerization, inhibiting Cell division is used to treat advanced breast cancer, non-small cell lung cancer and other tumor diseases. [0003] However, the water solubility of docetaxel is poor, and it is almost insoluble in water, and the prior art adopts Tween80 solubilization and ethanol solubilization to prepare a pharmaceutical preparation; due to the existence of Tween80, the preparation can cause allergic reactions, such as allergic reactions, Serious adverse reactions such as neurotoxicity; and after docetaxel enters the body, it is not selectively distribu...

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Problems solved by technology

[0003] But the water solubility of docetaxel is poor, almost insoluble in water, prior art adopts Tween80 solubilization, ethanol solubilization to make pharmaceutical preparation; Because the existence of Tween80 makes this preparation in clinical use process can cause as allergic reaction, Severe adverse reactions such as neurotoxicity; and after docetaxel enters the body, the distribution is non-selective and reaches various tissues and organs throughout the body, thereby causing systemic toxic and side effects, and easily causing toxicity to the nervous system and immune system, especially neutropenia Such as immune system toxicity, which greatly harms the physical and mental health of patients, which limits its clinical application; in addition, the stability of docetaxel is limited, and it must be used within 4 hours after clinical preparation, which limits the administration of docetaxel

[0004] At present, the existing technology solves the problem of poor water solubility of docetaxel by coating water-soluble polymer micelles on the surface of docetaxel, but its coating stability is still limited, and it will also be released suddenly when placed It is not highly resistant, it is inconvenient to apply, and it is easy to release suddenly after entering the body, which will bring systemic toxic and side effects; in addition, it is released too quickly after entering the body, and the therapeutic effect on tumor cells is not good.

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